Preparation method of micron hydrogel with colon-specific delivery

A hydrogel and specific technology, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems such as the greater influence on the activity of digestive enzymes, and reduce the inhibitory effect , good biocompatibility and degradability effects

Active Publication Date: 2020-07-28
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Puerarin has a good therapeutic effect on colon cancer and colitis clinically, but direct oral administration has a greater impact on the activity of digestive enzymes in the gastrointestinal tract

Method used

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  • Preparation method of micron hydrogel with colon-specific delivery
  • Preparation method of micron hydrogel with colon-specific delivery
  • Preparation method of micron hydrogel with colon-specific delivery

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Functional activity, biocompatibility and effect of puerarin on protease structure.

[0031] (1) Digest and count colon cancer cells (HCT116 cells) in logarithmic growth phase, adjust the initial concentration of cells to 1000 cells / well and 2000 cells / well, respectively inoculate into 96-well plates, place in 5% CO 2 After culturing in an incubator for 24 hours, the puerarin was formulated into 25, 50, 100, 200, 400, and 800 μg / mL solutions, and the puerarin solution was passed through a 0.22 μm water filter membrane. Use a pipette gun to suck out the 96-well plate cell supernatant culture solution and then add the above puerarin solution. The blank group is the blank complete medium without puerarin solution, continue to culture the cells, and use the MTT method to detect the cell viability after culturing for 72 hours and 48 hours respectively . The cell viability was obtained as figure 2 As shown in (a) and (b), the results in (a) show that the initial...

Embodiment 2

[0034] Embodiment 2: Preparation of micron hydrogel

[0035](1) Puerarin was placed in sterile distilled water and stirred until completely dissolved to prepare a puerarin solution (800 μg / mL). Afterwards, the low-methoxyl pectin was added to the puerarin solution and stirred until it was fully hydrated to prepare the continuous phase, and after the low-methoxyl pectin was fully hydrated, it was left standing to remove air bubbles. Chitosan solutions were prepared by dissolving chitosan completely in acetic acid solution (1% w / v). Zinc acetate was added to the chitosan solution and stirred for 2 hours to prepare a chitosan solution containing zinc acetate (5% w / v). Sorbitan monooleate (1% w / v) was added to liquid paraffin and stirred for 2 hours, then left to stand overnight to remove air bubbles for the preparation of the dispersed phase. All experiments were performed at room temperature.

[0036] (2) Use a pressure system to inject the continuous phase and the dispersed ...

Embodiment 3

[0041] Example 3: Research on Encapsulation Efficiency and Stability of Puerarin by Hydrogel

[0042] (1) use puerarin standard substance, adopt high performance liquid chromatography (HPLC) to establish standard curve, such as Image 6 Shown in (a) is the liquid chromatogram of puerarin standard substance. Pectinase and chitosanase hydrolyze the blank control group and micron hydrogel sample group loaded with puerarin, Image 6 (b) and (c) are the liquid chromatograms of the blank control group and the puerarin-loaded group, respectively. After the hydrogel was completely hydrolyzed, it was filtered through a 0.22 μm filter membrane, and the supernatant was subjected to high performance liquid chromatography to detect the content of puerarin. In this example, a Tuna C18(2) RP-HPLC system with 250x 4.6mm chromatographic column (Agilent1200, Shanghai, China). The column temperature used was 25° C., and the ratio of mobile phase methanol to water was 1:3. The detection wav...

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Abstract

The invention discloses a preparation method of micron hydrogel with colon-specific delivery. The preparation method comprises the following steps of dissolving puerarin and low-methoxy pectin in deionized water, carrying out stirring, dissolving, standing to remove bubbles, then sucking by using a microfluidic device water-phase sampler, and sucking mineral oil dissolved with span 80 by using anoil-phase sampler, wherein water-in-oil micron hydrogel generated by cutting of the microfluidic device flows out of the sample outlet and then enters a chitosan solution containing anhydrous zinc acetate, so that the pectin solution is demulsified and then is crosslinked with chitosan/zinc acetate. The micron hydrogel is used for embedding and releasing puerarin. The micron hydrogel prepared by the method has a colon-specific release effect.

Description

technical field [0001] The invention relates to a method for preparing a hydrogel, in particular to a method for preparing a micron hydrogel with colon-specific delivery. Background technique [0002] Puerarin has a good therapeutic effect on colon cancer and colitis clinically, but direct oral administration has a greater impact on the activity of digestive enzymes in the gastrointestinal tract. [0003] Low-methoxyl pectin has great advantages as a colon-targeted drug carrier, which can be specifically hydrolyzed by pectinase produced by colonic intestinal flora, thereby protecting the drug from being released in the gastrointestinal tract. Pectin is a kind of polygalacturonic acid polysaccharide. Low methoxyl pectin is generally produced from plant materials containing high-ester pectin, and the degree of esterification is less than 50%. Pectin is widely used in cosmetics, food and pharmaceutical preparations, and is non-toxic, so it can be used orally. [0004] Microfl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/36A61K31/352A61P1/00A61P35/00
CPCA61K9/0053A61K9/06A61K31/352A61K47/36A61P1/00A61P35/00
Inventor 袁彪程摇蓝曹崇江程抒劼王志祥
Owner CHINA PHARM UNIV
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